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    • 13. 发明授权
    • Indole derivatives
    • 吲哚衍生物
    • US4833153A
    • 1989-05-23
    • US928037
    • 1986-11-07
    • Michael D. DowleBrian EvansPeter Clark
    • Michael D. DowleBrian EvansPeter Clark
    • C07D209/16C07D403/06
    • C07D403/06C07D209/16
    • Compounds are disclosed of formula (I): ##STR1## wherein one of R.sup.1, R.sup.2 and R.sup.3 represents hydrogen, C.sub.1-6 alkyl C.sub.3-6 alkenyl, hydroxy, C.sub.1-4 alkoxy or a C.sub.2-5 alkoxycarbonyl group, a phenyl or substituted phenyl group or a phen(C.sub.1-4)alkyl or substituted phen(C.sub.1-4)alkyl group; and the other two each independently represents hydrogen, C.sub.1-6 alkyl, or R.sup.2 and R.sup.3 together form an alkylene chain --(CH.sub.2).sub.n --where n is 2 or 3, bridging the nitrogen atoms to which they are attached; R.sup.4 and R.sup.5, each independently represents hydrogen, C.sub.1-3 alkyl or propenyl; R.sup.6 represents hydrogen, C.sub.1-3 alkyl, and the physiologically acceptable salts and solvates thereof.The compounds (I) have potent and selective vasoconstrictor activity and are potentially useful for the treatment of migraine. The compounds (I) may be formulated in conventional manner as pharmaceutical compositions for administration by any convenient route.
    • 公开了式(I)的化合物:其中R 1,R 2和R 3中的一个表示氢,C 1-6烷基C 3-6烯基,羟基,C 1-4烷氧基或C 2-5烷氧基羰基, 苯基或取代的苯基或苯基(C 1-4)烷基或取代的苯基(C 1-4)烷基; 而另外两个独立地表示氢,C 1-6烷基或R 2和R 3一起形成亚烷基链 - (CH 2)n - ,其中n为2或3,桥接与它们相连的氮原子; R 4和R 5各自独立地表示氢,C 1-3烷基或丙烯基; R6代表氢,C1-3烷基及其生理上可接受的盐和溶剂合物。 化合物(I)具有有效和选择性的血管收缩剂活性,并且可用于治疗偏头痛。 化合物(I)可以以常规方式配制为用于通过任何方便途径给药的药物组合物。